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BMC Anesthesiology Jul 2021Liposomal bupivacaine (LB) is a long-acting formulation of bupivacaine. The safety and efficacy of LB has been demonstrated across surgical procedures. However,...
BACKGROUND
Liposomal bupivacaine (LB) is a long-acting formulation of bupivacaine. The safety and efficacy of LB has been demonstrated across surgical procedures. However, pharmacokinetic (PK) parameters and safety of LB in the Chinese population have not been assessed.
METHODS
In this single-arm, single center, phase 1, open-label study, PK and safety of local infiltration with LB 266 mg were assessed in healthy Chinese adults. Eligible participants were aged 18 to 55 years with biologic parents and grandparents of Chinese ethnicity, in generally good health (i.e., no clinically significant abnormalities), and with a body mass index (BMI) 19.0 to 24.0 kg/m (inclusive) and body weight ≥ 50 kg.
RESULTS
Participants (N = 20) were predominantly men (80 %); mean age was 32 years; and mean BMI was 21.8 kg/m. After LB administration, mean plasma levels of bupivacaine rapidly increased during the first hour and continued to increase through 24 h; plasma levels then gradually decreased through 108 h followed by a monoexponential decrease through 312 h. Geometric mean maximum plasma concentration was 170.9 ng/mL; the highest plasma bupivacaine concentration detected in any participant was 374.0 ng/mL. Twenty-two treatment-emergent adverse events were reported (mild, n = 21; moderate, n = 1).
CONCLUSIONS
After single-dose administration of LB, PK measures were similar to a previously reported profile in US adults. The highest observed peak plasma concentration of bupivacaine was several-fold below the plasma concentration threshold accepted as being associated with neurotoxicity or cardiotoxicity (2000-4000 ng/mL). These data support that LB is well tolerated and safe in individuals of Chinese descent.
TRIAL REGISTRATION
NCT04158102 (ClinicalTrials.gov identifier), Date of registration: November 5, 2019.
Topics: Adult; Anesthetics, Local; Asian People; Bupivacaine; Female; Humans; Liposomes; Male; Young Adult
PubMed: 34315419
DOI: 10.1186/s12871-021-01407-5 -
Anesthesiology Jan 2007Ropivacaine and levobupivacaine are local anesthetics that produce less motor block and greater sensory-motor separation when compared with equal milligram doses of... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Ropivacaine and levobupivacaine are local anesthetics that produce less motor block and greater sensory-motor separation when compared with equal milligram doses of bupivacaine. Although minimum local analgesic concentration studies suggested that they are less potent than bupivacaine, full dose-response studies have not been performed. The current trial describes the dose-response relation of levobupivacaine, ropivacaine, and bupivacaine, combined with sufentanil, when used for intrathecal labor analgesia.
METHODS
Four hundred fifty term parturients in active labor were included in this double-blind, randomized trial. Combined spinal-epidural anesthesia was performed, and ropivacaine, levobupivacaine, or bupivacaine was intrathecally administered in a dose of 1.0, 1.5, 2.0, 2.5, 3.0, or 3.5 mg, always combined with 1.5 microg sufentanil. Patients were considered responders to spinal analgesia if the visual analog scale score for pain was less than 25 mm within 15 min and the visual analog scale score remained less than 25 mm for 45 min. Patient demographics, obstetric data, maternal side effects, and fetal and neonatal well-being were noted. Group-specific dose-response curves were constructed using a probit regression model.
RESULTS
The ED95 of bupivacaine was 3.3 mg (95% confidence interval, 2.9-4.1). The ED95s of ropivacaine and levobupivacaine were 4.8 mg (95% confidence interval, 4.0-6.7) and 5.0 mg (95% confidence interval, 4.1-7.0), respectively. Racemic bupivacaine was significantly more potent than ropivacaine (P=0.0027) and levobupivacaine (P=0.0006). Ropivacaine and levobupivacaine were of similar potency (P=0.91).
CONCLUSIONS
This full dose-response study suggests that ropivacaine and levobupivacaine are of similar potency, whereas bupivacaine is more potent than both other drugs.
Topics: Adolescent; Adult; Amides; Analgesia, Epidural; Analgesia, Obstetrical; Anesthetics, Local; Bupivacaine; Dose-Response Relationship, Drug; Double-Blind Method; Female; Humans; Injections, Spinal; Levobupivacaine; Middle Aged; Pregnancy; Ropivacaine; Sufentanil
PubMed: 17197857
DOI: 10.1097/00000542-200701000-00024 -
Anesthesiology May 2024
Topics: Bupivacaine
PubMed: 38592361
DOI: 10.1097/ALN.0000000000004934 -
Anaesthesia Apr 2001Regional anaesthesia has seen the development of a new local anaesthetic: levobupivacaine. This review aims to outline the rationale underlying the development of... (Review)
Review
Regional anaesthesia has seen the development of a new local anaesthetic: levobupivacaine. This review aims to outline the rationale underlying the development of levobupivacaine and to consider its place in modern regional anaesthesia.
Topics: Anesthesia, Conduction; Anesthetics, Local; Animals; Bupivacaine; Humans; Stereoisomerism
PubMed: 11284819
DOI: 10.1046/j.1365-2044.2001.01964.x -
Journal of the American Academy of... May 2022Shoulder arthroscopy can result in substantial postoperative pain. Sucrose acetate isobutyrate extended-release bupivacaine (SABER-Bupivacaine; trade name Posimir) is a... (Randomized Controlled Trial)
Randomized Controlled Trial
INTRODUCTION
Shoulder arthroscopy can result in substantial postoperative pain. Sucrose acetate isobutyrate extended-release bupivacaine (SABER-Bupivacaine; trade name Posimir) is a novel depot formulation of bupivacaine designed to provide analgesia at the surgical site for up to 72 hours. The objective of this study was to evaluate the effect of SABER-Bupivacaine on pain and opioid consumption after arthroscopic subacromial decompression and to assess short-term and long-term safety.
METHODS
In this double-blind, placebo-controlled trial, 78 subjects were randomized in a 2:1 ratio to SABER-Bupivacaine 5 mL or SABER-placebo 5 mL injected into the subacromial space just before skin closure. Twenty-nine additional subjects were randomized on an exploratory basis to bupivacaine hydrochloride 20 mL, also injected subacromially. Subjects rated pain intensity on a 0 to 10 scale over the first 3 postoperative days and received intravenous or oral morphine for breakthrough pain. The coprimary efficacy end points were pain intensity on 90° shoulder flexion and cumulative morphine intake from 0 to 72 hours after surgery. The time to first use of opioid rescue analgesia was a secondary end point.
RESULTS
The mean (SD) pain intensity was 5.16 (1.94) for SABER-Bupivacaine and 6.43 (1.77) for placebo (P = 0.012). The median consumption of intravenous morphine equivalents was 4.0 mg for SABER-Bupivacaine and 12.0 mg for placebo (P = 0.010). The median time to first use of morphine rescue was 12.4 hours for SABER-Bupivacaine and 1.2 hours for placebo (P = 0.014). The corresponding values for bupivacaine hydrochloride were 5.16 (2.38), 8.0 mg, and 1.4 hours. The incidence and severity of treatment-emergent adverse events were similar for all treatment groups, and no functional or radiographic differences were noted at the 6-month follow-up.
DISCUSSION
Compared with placebo, SABER-Bupivacaine reduced pain and opioid analgesic consumption over 72 hours after arthroscopic subacromial decompression and prolonged the time to first use of opioid rescue analgesia. No safety signals were noted during the immediate postoperative period or at 6-month follow-up.
Topics: Analgesics, Opioid; Anesthetics, Local; Bupivacaine; Decompression; Humans; Morphine Derivatives; Pain, Postoperative
PubMed: 35584248
DOI: 10.5435/JAAOSGlobal-D-21-00287 -
Anesthesiology Jun 2010We have compared the pharmacokinetics and brain distribution of lidocaine, racemic bupivacaine (bupivacaine), and levobupivacaine in awake, spontaneously breathing rats. (Comparative Study)
Comparative Study
BACKGROUND
We have compared the pharmacokinetics and brain distribution of lidocaine, racemic bupivacaine (bupivacaine), and levobupivacaine in awake, spontaneously breathing rats.
METHODS
Lidocaine (0.5 mg x kg x min), bupivacaine (0.1 mg x kg x min), or levobupivacaine (0.1 mg x kg x min) was continuously administered to rats for 2 h (n = 12, each anesthetic). Blood samples and cerebral dialysate were collected during infusion and for 2 h after termination of infusion. Concentrations of anesthetics in the cerebral extracellular fluid were measured by microdialysis using the retrodialysis calibration method. Tissue-to-plasma partition coefficients calculated from the total (protein-bound and unbound) and unbound concentrations in plasma and brain as well as pharmacokinetic parameters in plasma and cerebral extracellular fluid were compared among the three anesthetics.
RESULTS
There were no differences in plasma total or unbound concentrations between bupivacaine and levobupivacaine. Concentrations of bupivacaine in the cerebral extracellular fluid were significantly higher than levobupivacaine (P < 0.001). Despite no differences in the ratio of total brain concentration to total plasma concentration among the three anesthetics, the ratio of cerebral extracellular fluid concentration to plasma unbound fraction of bupivacaine was significantly higher than lidocaine and levobupivacaine (0.58 +/- 0.09, 0.47 +/- 0.18, and 0.40 +/- 0.09, respectively; P = 0.03 and 0.003, respectively).
CONCLUSIONS
Although the ratio of total brain concentration to total plasma concentrations of lidocaine, bupivacaine, and levobupivacaine was similar, concentration ratio of bupivacaine in the cerebral extracellular fluid to plasma unbound fraction was significantly higher than lidocaine and levobupivacaine.
Topics: Animals; Brain; Bupivacaine; Dose-Response Relationship, Drug; Extracellular Fluid; Levobupivacaine; Lidocaine; Male; Rats; Rats, Sprague-Dawley; Wakefulness
PubMed: 20460991
DOI: 10.1097/ALN.0b013e3181d9cc54 -
Acta Cirurgica Brasileira Jul 2015To study racemic bupivacaine, non-racemic bupivacaine and ropivacaine on myocardial contractility. (Comparative Study)
Comparative Study
PURPOSE
To study racemic bupivacaine, non-racemic bupivacaine and ropivacaine on myocardial contractility.
METHODS
Isolated Wistar papillary muscles were submitted to 50 and 100 mM racemic bupivacaine (B50 and B100), non-racemic bupivacaine (NR50 and NR100) and ropivacaine (R50 and R100) intoxication. Isometric contraction data were obtained in basal condition (0.2 Hz), after increasing the frequency of stimulation to 1.0 Hz and after 5, 10 and 15 min of local anesthetic intoxication. Data were analyzed as relative changes of variation.
RESULTS
Developed tension was higher with R100 than B100 at D1 (4.3 ± 41.1 vs -57.9 ± 48.1). Resting tension was altered with B50 (-10.6 ± 23.8 vs -4.7 ± 5.0) and R50 (-14.0 ± 20.5 vs -0.5 ± 7.1) between D1 and D3. Maximum rate of tension development was lower with B100 (-56.6 ± 38.0) than R50 (-6.3 ± 37.9) and R100 (-1.9 ± 37.2) in D1. B50, B100 and NR100 modified the maximum rate of tension decline from D1 through D2. Time to peak tension was changed with NR50 between D1 and D2.
CONCLUSIONS
Racemic bupivacaine depressed myocardial contractile force more than non-racemic bupivacaine and ropivacaine. Non-racemic and racemic bupivacaine caused myocardial relaxation impairment more than ropivacaine.
Topics: Amides; Anesthetics, Local; Animals; Bupivacaine; Depression, Chemical; Male; Muscle Tonus; Myocardial Contraction; Papillary Muscles; Rats, Wistar; Reference Values; Ropivacaine; Stereoisomerism; Time Factors
PubMed: 26270140
DOI: 10.1590/S0102-865020150070000006 -
Pain Research & Management 2021Brachial plexus block is frequently recommended for upper limb surgeries. Many drugs have been used as adjuvants to prolong the duration of the block. This study aimed...
BACKGROUND
Brachial plexus block is frequently recommended for upper limb surgeries. Many drugs have been used as adjuvants to prolong the duration of the block. This study aimed to assess the effect of dexmedetomidine with bupivacaine combination and only bupivacaine on sensory and motor block duration time, pain score, and hemodynamic variations in the supraclavicular block in upper extremity orthopedic surgery.
METHODS
This prospective, double-blind clinical trial study was conducted on 60 patients, 20 to 60 years old. Patients were candidates for upper extremity orthopedic surgeries. The sensory and motor block were evaluated by using the pinprick method and the modified Bromage scale. The postoperative pain was assessed by utilizing a visual analog scale.
RESULTS
The mean onset time of sensory and motor block in patients receiving only bupivacaine was, respectively, 31.03 ± 9.65 min and 24.66 ± 9.2 min, and in the dexmedetomidine receiving group, it was about 21.36 ± 8.34 min and 15.93 ± 6.36 minutes. The changes in heart rate and mean arterial blood pressure were similar in both groups. The duration of sensory and motor block and the time of the first analgesia request in the intervention group were longer. Postoperative pain was lower in the intervention group for 24 hours ( = 0.001).
CONCLUSION
Dexmedetomidine plus bupivacaine reduced the onset time of sense and motor blocks and increased numbness and immobility duration. Also, dexmedetomidine reduced postoperative pain significantly with the use of bupivacaine for supraclavicular blocks. . IRCT, IRCT20160430027677N15. Registered 05/28/2019, https://www.irct.ir/trial/39463.
Topics: Adult; Brachial Plexus Block; Bupivacaine; Dexmedetomidine; Double-Blind Method; Female; Humans; Hypnotics and Sedatives; Male; Middle Aged; Prospective Studies; Young Adult
PubMed: 33927790
DOI: 10.1155/2021/8858312 -
Pain Research & Management 2022Comparing bupivacaine's adjuvants in spinal anesthesia, we assessed the specific blocking characteristics and adverse effects of bupivacaine alone and in combination... (Randomized Controlled Trial)
Randomized Controlled Trial
Analgesic Characteristics of Bupivacaine Alone and in Combination with Dexmedetomidine or Meperidine in Spinal Anesthesia during Cesarean Section: A Double-Blind Randomized Clinical Trial Study.
BACKGROUND
Comparing bupivacaine's adjuvants in spinal anesthesia, we assessed the specific blocking characteristics and adverse effects of bupivacaine alone and in combination with dexmedetomidine or meperidine in spinal anesthesia during cesarean section.
METHODS
In this double-blind randomized clinical trial study, ninety pregnant women were divided into groups to receive 10 mg bupivacaine (group B), 10 mg bupivacaine with 5 g dexmedetomidine (group BD), or 10 mg bupivacaine with 10 mg meperidine (group BM) intrathecal. Patients were assessed for the quality of analgesia during operations. Durations of sensory and motor blocks and anesthesia-related complications were analyzed using SPSS 21, and values <0.05 were considered statistically significant.
RESULTS
The onset of sensory and motor blocks was essentially the same in all treated groups. Block regression time was significantly prolonged in the BD group compared to the B and BM groups ( < 0.001). The duration of analgesia was significantly longer in the BD and BM groups than in the B group ( < 0.001). The level of sedation in the BD group was higher than in the B group. Shivering occurred in 40% of patients in the B group, which was significantly more than that of the BD (16.6%) and BM (33.3%) groups. Itching happened in 33.3% of women in the BM group which was statistically more than that of the B (3.33%) and BD (0) groups. The incidence of adverse effects was the same in all groups.
CONCLUSION
The combination of bupivacaine with dexmedetomidine significantly prolonged sensory and motor regression time and duration of analgesia.
Topics: Analgesics; Anesthesia, Spinal; Anesthetics, Local; Bupivacaine; Cesarean Section; Dexmedetomidine; Double-Blind Method; Female; Humans; Injections, Spinal; Meperidine; Pain; Pregnancy
PubMed: 35899020
DOI: 10.1155/2022/5111214 -
Iranian Journal of Medical Sciences Jul 2023Several adjuvants, added to local anesthetics, were suggested to induce an ideal regional block with high-quality analgesia. The purpose of this study was to evaluate... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Several adjuvants, added to local anesthetics, were suggested to induce an ideal regional block with high-quality analgesia. The purpose of this study was to evaluate the particular blocking properties of low-dose bupivacaine in combination with meperidine and fentanyl in spinal anesthesia during Cesarean sections.
METHODS
A randomized, double-blind clinical trial was conducted at Hafez Hospital affiliated with Shiraz University of Medical Sciences (Shiraz, Iran) from February 2015 to February 2016. A total of 120 pregnant women, who underwent spinal anesthesia during elective Cesarean section were enrolled in the study. Based on block-wise randomization, the patients were randomly assigned to three groups, namely "B" group received 2 mL bupivacaine 0.5% (10 mg), "BM" group received 8 mg bupivacaine and 10 mg meperidine, and "BF" group received 8 mg bupivacaine and 15 µg fentanyl intrathecally. The block onset, the duration of analgesia, and the time of discharge from the post-anesthesia care unit (PACU) were all assessed. Data were analyzed using SPSS software version 21, and P<0.05 were considered statistically significant.
RESULTS
The mean duration of motor blocks in the B group (150 min) were significantly higher than the BM (102 min) and BF (105 min) groups (P<0.0001). In both the BM and BF groups, the duration of sensory and motor blocks was the same. The length of stay in the PACU was significantly longer in the B group (P<0.001) than the BM and BF groups. When meperidine or fentanyl was added to bupivacaine, the duration of the analgesia lengthened (P<0.001).
CONCLUSION
Intrathecal low-dose spinal anesthesia induced by bupivacaine (8 mg) in combination with meperidine and/or fentanyl for Cesarean section increased maternal hemodynamic stability, while ensuring effective anesthetic conditions, extending effective analgesia, and reducing the length of stay in PACU. IRCT2015013119470N14.
Topics: Humans; Female; Pregnancy; Bupivacaine; Cesarean Section; Fentanyl; Anesthesia, Spinal; Analgesia; Meperidine
PubMed: 37456203
DOI: 10.30476/IJMS.2022.95205.2653